CB-839 (Synonyms: Telaglenastat) |
Catalog No.GC15227 |
CB-839(CB-839)는 동급 최초의 선택적이고 가역적인 경구 활성 글루타미나제 1(GLS1) 억제제입니다. CB-839는 GLS2와 비교하여 GLS1 스플라이스 변이체 KGA(신장형 글루타미나제) 및 GAC(글루타미나제 C)를 선택적으로 억제합니다. IC50은 마우스 신장 및 뇌의 내인성 글루타미나아제에 대해 각각 23nM 및 28nM입니다. CB-839는 자가포식을 유도하고 항종양 활성이 있습니다.
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Cas No.: 1439399-58-2
Sample solution is provided at 25 µL, 10mM.
Telaglenastat (CB-839) is a first-in-class, reversible and orally bioavailable glutaminase 1 (GLS1) inhibitor. Telaglenastat (CB-839) selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Antitumor activity[1].
Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s of 49 nM and 26 nM, respectively[1].Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells[1].
Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1].
References:
[1]. Gross MI, et al. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901.
[2]. Biancur DE, et al. Compensatory metabolic networks in pancreatic cancers upon perturbation of glutaminemetabolism. Nat Commun. 2017 Jul 3;8:15965.
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